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键合紫杉醇和姜黄素的金纳米棒的制备及体外抗肿瘤多药耐药研究
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篇名: 键合紫杉醇和姜黄素的金纳米棒的制备及体外抗肿瘤多药耐药研究
TITLE:
摘要: 目的:制备键合紫杉醇(PTX)和姜黄素(CUR)的金纳米棒(GNR)(PTX/CUR-BPGNR),并初步研究其体外抗肿瘤多药耐药(MDR)作用及机制。方法:用晶种生长法制备GNR,然后经生物素-聚乙二醇修饰制成GNR(BPGNR)。分别合成PTX和CUR的硫辛酸酯(PTXLA和CURLA),使用核磁共振氢谱(1H-NMR)和质谱等手段确定其化学结构。利用金硫键牢固的结合作用,将PTXLA和CURLA连接到BPGNR表面,得到键合PTX和CUR的BPGNR(PTX/CUR-BPGNR)。观察其形貌,考察其载药量和体外释药情况(近红外光照和酯酶条件下)。以阿霉素(ADR)的MDR人乳腺癌细胞MCF-7/ADR为研究对象,分别经PTX、CUR、PTX/CUR混合物和PTX/CUR-BPGNR处理后,采用MTT法考察MCF-7/ADR细胞的存活率,酶联免疫吸附测定法检测细胞中P-糖蛋白(P-gp)表达水平。结果:成功制得PTX/CUR-BPGNR,其大小、形状均一,最大吸取波长为808 nm,其中PTX和CUR的载药量分别为16.1%、8.4%,同时给予近红外光照和酯酶能促进PTX和CUR释放,64 h的累积释放度分别可达37.2%、39.1%。BPGNR、PTX、CUR、PTX/CUR混合物和PTX/CUR-BPGNR处理后MCF-7/ADR细胞的存活率分别为95.8%、71.2%、91.9%、45.8%、22.5%,细胞中P-gp的相对表达水平分别为105.6%、75.2%、73.8%、51.7%。结论:成功制得PTX/CUR-BPGNR,其可提高CUR抑制P-gp表达的能力,从而增强药物抗MDR的作用。
ABSTRACT: OBJECTIVE: To prepare paclitaxel(PTX) and curcumin (CUR) chemically conjugated gold nanorod (GNR) (PTX/CUR-BPGNR), and to preliminarily study its anti-multidrug-resistant(MDR) tumor effect in vitro and mechanisms. METHODS: GNR was prepared by seed growth method and modified with biotin-polyethylene glycol (Biotin-PEG) to obtain BPGNRs. Lipoic acid PTX and CUR (PIXLA and CURLA) were synthesized; 1H-NMR and MS were used to confirm their chemical structures. PTXLA and CURLA were connected to BPGNR surface to obtain PIX and CUR-bonding BPGNR (PTX/CUR-BPGNR) via strong binding of Au-S bond. The morphology of PTX/CUR-BPGNR was observed, and drug-loading amount and in vitro drug release were investigated (under near-infrared illumination and esterase condition). Adriamycin (ADR) MDR breast cancer MCF-7/ADR cells were selected as research objects, and MTT assay was used to investigate the survival rate of cells after treated with BPGNR, PTX, CUR, PTX/CUR mixture and PTX/CUR-BPGNR, and ELISA was used to detect the expression of P-gp. RESULTS: PTX/CUR-BPGNR was prepared successfully with uniform size and shape. The maximum absorption wavelength was 808 nm, and drug-loading amount of PTX and CUR were 16.1% and 8.4%, respectively. The preparations were given near-infrared illumination and esterase to promote the release of PTX and CUR. 64 h accumulative drug release rates were 37.2% and 39.1%. Survival rates of MCF-7/ADR cells after treated with BPGNR, PTX, CUR and PTX/CUR mixture, PTX/CUR-BPGNR were 95.8%, 71.2%, 91.9%, 45.8% and 22.5%, respectively. The relative expressions of P-gp in cells were 105.6%, 75.2%, 73.8%, 51.7%, respectively. CONCLUSIONS: PTX/CUR-BPGNR is successfully prepared and can improve the ability of CUR inhibiting the expression of P-gp so as to strengthen its anti-MDR effects.
期刊: 2018年第29卷第15期
编辑: 徐绍辉,张志鹏,黄胜堂,沈园园,于坤宏
AUTHORS: XU Shaohui,ZHANG Zhipeng,HUANG Shengtang,SHEN Yuanyuan,YU Kunhong
关键字: 紫杉醇;姜黄素;金纳米棒;抗肿瘤多药耐药;P-糖蛋白
KEYWORDS: Paclitaxel; Curcumin; Gold nanorods; Multidrug resistant cancer; P-gp
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